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تعداد آیتم قابل مشاهده باقیمانده : -14 مورد

Dosing and administration of long-acting injectable antipsychotics for schizophrenia in adults

Dosing and administration of long-acting injectable antipsychotics for schizophrenia in adults
Drug and route Brand name Injection interval Available dose strengths Maximum dose Initiation and conversion from oral therapy Injection site and technique Solubilization and vehicle
Second-generation
Aripiprazole (IM) Abilify Maintena 4 weeks

300 mg

400 mg

400 mg every 4 weeks

Single injection start: Overlap with oral aripiprazole (or other oral antipsychotic) for 14 days after first LAI dose. Initiate LAI with 400 mg every 4 weeks.

or

Alternative double injection start:[1] Two injections of 400 mg (at different sites) administered concurrently with a single dose of 20 mg oral aripiprazole, followed by 400 mg IM every 4 weeks*.

Deltoid or gluteal; standard IM injection Low solubility particles in aqueous suspension
Abilify Asimtufii 8 weeks

720 mg

960 mg

960 mg every 8 weeks

Overlap with oral aripiprazole (or other oral antipsychotic) for 14 days after first LAI dose. Initiate LAI with 960 mg every 8 weeks.

If switching from 4-week aripiprazole LAI (Abilify Maintena), administer first dose of 960 mg in place of next scheduled injection; do not overlap with oral treatment.

Gluteal; standard IM injection Low solubility particles in aqueous suspension
Aripiprazole lauroxil (IM) Aristada 4, 6, or 8 weeks (dose dependent)

441 mg

662 mg

882 mg

1064 mg

882 mg every 4 weeks 21-day oral overlap start: Overlap with oral aripiprazole for 21 days after the first LAI dose; starting LAI dose is based on oral aripiprazole dose as follows:
  • Oral dose of 10 mg/day:
    • 441 mg LAI every 4 weeks.
  • Oral dose of 15 mg/day, choose 1 of the following:
    • 662 mg LAI every 4 weeks.
    • 882 mg LAI every 6 weeks.
    • 1064 mg LAI every 8 weeks.
  • Oral dose ≥20 mg/day:
    • 882 mg LAI every 4 weeks.

or

1-day oral overlap start (using Aristada Initio): Single dose of 30 mg oral aripiprazole plus a one-time 675 mg Aristada Initio loading dose; may be given on same day or up to 10 days prior to first maintenance aripiprazole lauroxil LAI dose (based on oral dose using conversion above) with no additional oral overlap.

Gluteal (441 mg dose may also be administered in the deltoid); standard IM injection Low solubility particles in aqueous suspension
Aristada Initio nanocrystal dispersion (for optional loading dose or re-initiation after missed doses only) Once 675 mg N/A Deltoid or gluteal; standard IM injection Nanoparticles in aqueous suspension
Olanzapine pamoate (IM) Zyprexa Relprevv 2 or 4 weeks (dose dependent)

210 mg

300 mg

405 mg

300 mg every 2 weeks or 405 mg every 4 weeks No oral overlap required; starting LAI dose is based on stable dose of oral olanzapine as follows:
  • Oral dose of 10 mg/day:
    • First 8 weeks: 210 mg LAI every 2 weeks or 405 mg LAI every 4 weeks.
    • Thereafter: 150 mg LAI every 2 weeks or 300 mg LAI every 4 weeks.
  • Oral dose of 15 mg/day:
    • First 8 weeks: 300 mg LAI every 2 weeks.
    • Thereafter: 210 mg LAI every 2 weeks or 405 mg LAI every 4 weeks.
  • Oral dose of 20 mg/day:
    • 300 mg LAI every 2 weeks.
Gluteal; standard IM injection Nanoparticles in aqueous suspension
Paliperidone palmitate (IM)Δ Invega Sustenna; Erzofri (4-week) 4 weeks

39 mg

78 mg

117 mg

156 mg

234 mg

351 mg (Erzofri loading dose only)

234 mg every 4 weeks

No oral overlap required.

Loading dose:

  • Invega Sustenna: 234 mg LAI on treatment day 1 followed by 156 mg LAI 1 week later.
  • Erzofri: 351 mg LAI on treatment day 1.

Maintenance dose: Initiate 4 weeks after loading dose is complete (5 weeks after first Invega Sustenna dose); dose is based on stable dose of oral extended-release paliperidone as follows:

  • Oral dose of 3 mg/day: 39 or 78 mg LAI every 4 weeks.
  • Oral dose of 6 mg/day: 117 mg LAI every 4 weeks.
  • Oral dose of 9 mg/day: 156 mg LAI every 4 weeks.
  • Oral dose of 12 mg/day: 234 mg LAI every 4 weeks.
Deltoid (load or maintenance) or gluteal (maintenance only); standard IM injection Nanoparticles (Invega Sustenna) or low solubility particles (Erzofri) in aqueous suspension
Invega Trinza (12-week) 12 weeks (3 months)

273 mg

410 mg

546 mg

819 mg

819 mg every 12 weeks Use only after adequate treatment and dose has been established with paliperidone palmitate 4-week LAI suspension for ≥4 months; the last two 4-week injection cycles should be the same dose before initiation. Dose is based on last dose of paliperidone palmitate 4-week LAI and is administered at the time the next dose is due as follows:
  • For 4-week LAI dose of 78 mg, use 273 mg 12-week LAI.
  • For 4-week LAI dose of 117 mg, use 410 mg 12-week LAI.
  • For 4-week LAI dose of 156 mg, use 546 mg 12-week LAI.
  • For 4-week LAI dose of 234 mg, use 819 mg 12-week LAI.
  • Conversion from 4-week LAI dose of 39 mg was not studied.
Deltoid or gluteal; standard IM injection Nanoparticles in aqueous suspension
Invega Hafyera (6-month) 6 months

1092 mg

1560 mg

1560 mg every 6 months Use only after adequate treatment and dose has been established with paliperidone palmitate 4-week LAI for a minimum of 4 months (the last two 4-week injection cycles should be the same dose before initiating) or paliperidone palmitate 12-week LAI for 1 cycle (3 months). Dose is based on last dose of paliperidone 4- or 12-week LAI and is administered at the time the next dose is due as follows:
  • For 4-week LAI dose of 156 mg, use 1092 mg 6-month LAI.
  • For 4-week LAI dose of 234 mg, use 1560 mg 6-month LAI.
  • For 12-week LAI dose of 546 mg, use 1092 mg 6-month LAI.
  • For 12-week LAI dose of 819 mg, use 1560 mg 6-month LAI.
  • Conversion from 4-week LAI doses of 39, 78, or 117 mg or 12-week LAI doses of 273 or 410 mg were not studied.
Gluteal; standard IM injection Low solubility particles in aqueous suspension
Risperidone (IM) Risperdal consta; Rykindo 2 weeks

12.5 mg

25 mg

37.5 mg

50 mg

50 mg every 2 weeks Overlap with full-dose oral treatment for first 3 weeks (Risperdal Consta) or first week (Rykindo); starting LAI dose is based on stable dose of oral risperidone as follows:
  • Oral dose of ≤3 mg/day: 25 mg LAI every 2 weeks.
  • Oral dose of >3 to ≤5 mg/day: 37.5 mg LAI every 2 weeks.
  • Oral dose of >5 mg/day: 50 mg LAI every 2 weeks.
Deltoid (Risperdal Consta only) or gluteal; standard IM injection Microsphere matrix in aqueous suspension
Risvan 4 weeks

75 mg

100 mg

100 mg every 4 weeks No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
  • Oral dose of 3 mg/day: 75 mg LAI every 4 weeks.
  • Oral dose of 4 mg/day: 100 mg LAI every 4 weeks.
Deltoid or gluteal; standard IM injection Suspended in copolymer solution
Risperidone (SUBQ) Perseris 4 weeks

90 mg

120 mg

120 mg every 4 weeks No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
  • Oral dose of 3 mg/day: 90 mg LAI every 4 weeks.
  • Oral dose of 4 mg/day: 120 mg LAI every 4 weeks.
Abdomen or back of the upper arm; SUBQ injection Suspended in polymer solution
Uzedy 4 or 8 weeks (dose dependent)

50 mg

75 mg

100 mg

125 mg

150 mg

200 mg

250 mg

125 mg every 4 weeks or 250 mg every 8 weeks No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
  • Oral dose of 2 mg/day: 50 mg LAI every 4 weeks or 100 mg LAI every 8 weeks.
  • Oral dose of 3 mg/day: 75 mg LAI every 4 weeks or 150 mg LAI every 8 weeks.
  • Oral dose of 4 mg/day: 100 mg LAI every 4 weeks or 200 mg LAI every 8 weeks.
  • Oral dose of 5 mg/day: 125 mg LAI every 4 weeks or 250 mg LAI every 8 weeks.
Abdomen or back of the upper arm; SUBQ injection Suspended in copolymer solution
First-generation
Flupentixol decanoate (IM)§ Fluanxol Depot Variable; typically 2 to 4 weeks

20 mg/mL

100 mg/mL

100 mg every 2 weeks

Overlap with oral treatment at descending doses for first week; initiate LAI at 4 times daily oral dose every 2 weeks or 8 times daily oral dose every 4 weeks.

Usual dose range: 10 to 50 mg.

Gluteal or lateral thigh¥; Z-track IM injection Ester in medium chain triglycerides or coconut oil
Fluphenazine decanoate (IM) Prolixin decanoate Variable; typically 2 to 4 weeks 25 mg/mL 100 mg every 2 weeks Initial 6.25 to 25 mg or use the following conversion from oral fluphenazine:
  • 1 mg oral fluphenazine is approximately 1.25 mg LAI every 3 weeks.

Overlap with oral therapy at one-half daily oral dose following the first injection; may discontinue oral therapy at time of the second injection.

Usual dose range: 6.25 to 100 mg.

Gluteal; Z-track IM Ester in sesame seed oil
Haloperidol decanoate (IM) Haldol decanoate 3 or 4 weeks

50 mg/mL

100 mg/mL

450 mg every 4 weeks The first haloperidol decanoate LAI dose should not exceed 100 mg; if larger doses are required based on oral dose conversion, administer the first dose in two separate injections with 100 mg administered on day 1 and the remainder administered in 3 to 7 days. If the total dose ≥400 mg, it is given in a series of 3 injections. Subsequent doses may be administered as a single injection. Options for initiation include the following:
  • Regimen without oral overlap:
    • First dose: Initiate LAI at 20 times the oral daily dose.
    • Second dose (at 4 weeks): Reduce initial LAI dose by approximately 25%.
    • Maintenance dose (at 8 weeks and every 4 weeks thereafter): Reduce to approximately 50% of the initial LAI dose.
    • Dose reductions in months 2 and 3 may be modified as needed based upon clinical response.
  • Regimen with oral overlap: Initiate LAI at the anticipated maintenance dose of 10 to 15 times the daily oral dose. Overlap with oral treatment for 1 month then gradually taper oral dose (eg, by 25% per week) over a 1-month period beginning 1 to 2 months after the first LAI dose.

Usual dose range: 50 to 200 mg (10 to 15 times previous oral dose).

Gluteal; Z-track IM injection Ester in sesame seed oil
Zuclopenthixol decanoate (IM)§ Clopixol Depot 2 to 4 weeks 200 mg/mL (variable; usual dose range: 100 to 400 mg) 600 mg every 2 weeks Oral overlap with tapering may be considered during transition; starting LAI dose is based on stable dose of oral zuclopenthixol as follows:
  • Oral dose of ≤20 mg/day: 100 mg LAI every 2 weeks.
  • Oral dose of 25 to 40 mg/day: 200 mg LAI every 2 weeks.
  • Oral dose of 50 to 75 mg/day: 300 mg LAI every 2 weeks.
  • Oral dose of >75 mg/day: 400 mg LAI every 2 weeks.
Gluteal or lateral thigh¥; Z-track IM injection Ester in low viscosity 20% vegetable oil
  • Long-acting preparations are administered by deep intramuscular (IM) administration and never given intravenously. SUBQ administration of IM labeled formulations is not recommended due to variable absorption and increased risk of local site reaction, except specific formulations approved for SUBQ administration (eg, risperidone subcutaneous [Perseris, Uzedy]).
  • Significant dose reduction or avoidance may be required for older or debilitated adults, patients with low cardiac output or kidney or liver impairment, and for drug interactions or known poor CYP2D6 metabolizer (eg, aripiprazole). For additional information, refer to Lexidrug monographs available in UpToDate and/or local prescribing information.
  • Details shown are specific to preparations available in the United States, unless otherwise noted.

CYP: cytochrome P450; IM: intramuscular; LAI: long-acting injectable (also known as "depot" injection); SUBQ: subcutaneous.

* Aripiprazole double injection (ie, two IM doses of 400 mg each at separate sites) is off-label in the United States but is approved in other countries.[1]

¶ A lower starting dose of 150 mg every 4 weeks may be used in patients who are debilitated, at risk for orthostatic hypotension, or may metabolize more slowly (eg, nonsmoking, female, ≥65 years of age).

Δ Paliperidone LAI dosing in the United States labeling is based on paliperidone palmitate; dosing in some other areas (eg, Canada, United Kingdom, European Union) is based on paliperidone base (paliperidone palmitate 1 mg is equivalent to paliperidone base approximately 0.64 mg); refer to local product labeling.

◊ Rykindo is not a generic equivalent to Risperdal Consta; it has a more rapid onset. If switching from Risperdal Consta to Rykindo, initiate at same dose starting 4 weeks after the last injection; do not overlap with oral treatment.

§ Not available in the United States. Product details are from Health Canada product monographs.

¥ Lateral thigh administration is off-label in Canada, but is approved in other countries.

‡ Although SUBQ administration is described in the United States label, UpToDate contributors avoid SUBQ use. The required injection volumes (eg, >1.5 mL for doses >37.5 mg) may not be well tolerated.

† Alternatively, fluphenazine and haloperidol LAI may be given in the deltoid based upon clinical experience. For deltoid administration, use of a 23-gauge, 1-inch needle is appropriate for most adults; volume per injection is typically limited to 1 mL at this site. Deltoid administration is off-label and published clinical data are unavailable.

Data from UpToDate Lexidrug. More information available at https://online.lexi.com/.

Reference:

  1. Aripiprazole for prolonged release injectable suspension. Health Canada-approved product monograph. Revised March, 2021. Health Canada. (Available online at https://health-products.canada.ca/dpd-bdpp/index-eng.jsp; accessed April 10, 2024.)
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